PRODURG, MEDICINAL UTILIZATION THEREOF AND PROCESS FOR PRODUCING THE SAME

摘要

A prodrug with the use of an enzyme showing different enzymatic activities between a drug target site and a site where its side effect is expressed, which has a substituent cleavable with the enzyme and is activated due by cleaving the substituent. As an example of the drug target site, a respiratory organ may be cited, while the heart may be sited as an example of the side effect expression site. As an example of the drug, a bronchodilator may be cited while a glicosidase (for example, beta-glucuronidase) may be cited as an example of the enzyme. As an example of the substituent, a glycosyl group comprising a monosaccharide or an oligosaccharide may be cited. Use of the above enzyme makes it possible to lessen the side effect of a drug having a target site for exerting its effect which is different from a site where its side effect is expressed.